Pharmacology Flashcards
pirfenidone
inhibits TGF-beta mediated collagen synthesis
tx for IPF
decreased rate of FVC decline, may decrease mortality
side fx: nausea, photosensitivity, rash, dyspepsia, elevated LFTs
nintedanib
multiple tyrosine kinase inhibitor
tx for IPF
decreased rate of FVC decline, may decrease exacerbations
side fx: nausea, vomiting, elevated LFTs
steps of asthma management, GINA guidelines?
- watch pt use inhaler, discuss adherence/barriers
- confirm dx asthma
- remove RF if possible, assess/manage comorbidities
- tx step up
- refer to specialist`
what are the two classes of beta agonists?
short acting (rescue inhlaer) and long acting (daily controller)
mechanism of beta agonists?
GPCRs activate adenylyl cyclase –> convert ATP to cAMP –> cause bronchodilation
increase vasodilation, bronchodilation, liver glycogenolysis.
side fx tachycardia, anxiety
do we need to worry about beta receptor cross over effects?
nope!
LABA and LAMA are first line therapy for what disease?
COPD
can use only one or both
are LABA and LAMA first line therapy for asthma
NO. only after ICS
why is LABA/LAMA NOT first line therapy for asthma?
risk of exacerbations.
note: together there is better control of asthma. great as add on therapy in addition to ICS
what is the mechanism of action of muscarinic receptor antagonists?
ACh binds muscarinic and nicotinic receptors.
reversibly inhibit effects of ACh on M3 muscarinic receptor –> causes bronchodilation
what are side effects of anti cholinergic drugs?
unilateral dilated pupil bc getting out from mask
imp: should see if on other anticholinergic meds bc increase risk of side effects
flushing, confusion, hyperthermia, dry mouth, urinary retention, tachycardia
is there a role for anticholinergics in asthma management?
as alternative salvage therapy
what is the mechanism of inhaled corticosteroids?
bind glucocorticoid receptor in cytoplasm and enter nucleus to act as TF for antiinflammatory effects.
decrease inflammatory signals and cells. decrease mucus secretion and leakage from endothelium. increase beta2 receptors on airway smooth muscle
what is frontline tx for asthma?
low dose ICS
what is an important adverse effect of ICS?
thrush
also increased risk of pneumonia, hoarse voice, skin bruising
can ICS be used in COPD?
yes if ongoing sxs despite LABA/LAMA
what is the mechanism of leukotriene antagonists?
zileuton: selective and specific 5-lipoxygenase inhibitor. prevents conversion of arachidonic acid to leukotriene A4
montelukast and zafirlukast: selective, reversible antagonists of cysteinyl leukotriene-1-receptor, blocks final step in leukotriene pathway
prevent leukotriene pathway which promotes smooth muscle constriction, eosinophil migration, and edema
why do doctors like montelukast?
broad indications (children >1 year old) minimal drug drug interactions favorable side effect profile
what patients would receive leukotriene receptor antagonists?
asthma pts as add on therapy
what is the mech of action for phosphodiesterase-4 inhibitors (rofumilast)?
prevent breakdown of cAMP
this decreases inflamm cell activity, inhibits fibrosis, and relaxes smooth muscle
who gets phosphodiesterase-4 inhibitors (rofumilast)?
late stage COPD pts. if LAMA/LABA/ICS still have frequent exacerbations
not used in asthma
side effects of rofumilast (PDE-4 inhib)
GI related
indications for theophylline?
asthma pts as add on therapy
narrow therapeutic window and can cause fatal arrythmias and seizures at toxic levels
(also called methylxanthine- nonselective PDE inhibitor)
Bupropion (aka wellbutrin)
blocks neural reuptake of dopamine and/or norepi
contraindicated in pts with seizure hx
start at least 7 days before quit date
